Pharmacokinetic evaluation of transdermal buprenorphine in man

被引:10
作者
Wilding, IR
Davis, SS
Rimoy, GH
Rubin, P
KuriharaBergstrom, T
Tipnis, V
Berner, B
Nightingale, J
机构
[1] QUEENS MED CTR,DEPT THERAPEUT,NOTTINGHAM NG7 2UH,ENGLAND
[2] CIBA GEIGY CORP,ARDSLEY,NY 10502
关键词
buprenorphine; transdermal; pharmacokinetic evaluation; man;
D O I
10.1016/0378-5173(96)85198-2
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Transdermal delivery of the synthetic opiate analgesic, buprenorphine, was studied in healthy volunteers. Pharmacokinetic, safety and tolerability data were obtained in a group of 12 healthy subjects following administration of a short intravenous infusion and the application of both aqueous- and ethanol-based fillable transdermal therapeutic systems (FTTS), containing 8 and 37.5 mg of drug, respectively. The total amount delivered by the 10 cm(2) aqueous reservoir system ranged from 0.11 to 0.67 mg over the 24 h application period and the steady state in vivo flux rates were 0.56-1.91 mu g/cm(2)/h. The total amount delivered by the 5 cm(2) ethanol-based FTTS ranged from 0.33 to 0.96 mg and the steady state in vivo flux values were 2.14-5.62 mu g/cm(2)/h. The results of the feasibility investigation demonstrated that transdermal delivery of buprenorphine produced sustained plasma levels of drug within the range observed after intravenous dosing and that an ethanolic formulation produced approximately a four-fold increase in transdermal flux. The in vivo investigation suggests that transdermal delivery could provide appropriate plasma levels of buprenorphine for sustained analgesic effect.
引用
收藏
页码:81 / 87
页数:7
相关论文
共 16 条
[1]  
ADRIAENSEN H, 1985, ACTA ANAESTH BELG, V1, P33
[2]   ALTERNATE-DAY DOSING DURING BUPRENORPHINE TREATMENT OF OPIOID DEPENDENCE [J].
AMASS, L ;
BICKEL, WK ;
HIGGINS, ST ;
BADGER, GJ .
LIFE SCIENCES, 1994, 54 (17) :1215-1228
[3]   BUPRENORPHINE KINETICS [J].
BULLINGHAM, RES ;
MCQUAY, HJ ;
MOORE, A ;
BENNETT, MRD .
CLINICAL PHARMACOLOGY & THERAPEUTICS, 1980, 28 (05) :667-672
[4]   BUPRENORPHINE - NEW POTENT LONG-ACTING SYNTHETIC ANALGESIC - COMPARISON WITH MORPHINE [J].
DOWNING, JW ;
LEARY, WP ;
WHITE, ES .
BRITISH JOURNAL OF ANAESTHESIA, 1977, 49 (03) :251-255
[5]  
GRANGER CD, 1991, Patent No. 432945
[6]  
HAMBROOK JM, 1976, OPIATES ENDOGENOUS O, P295
[7]  
HIDAKA O, 1991, Patent No. 9116044
[8]  
HILLE T, 1991, Patent No. 3939376
[9]  
JASINSKI DR, 1978, ARCH GEN PSYCHIAT, V35, P501
[10]   BUPRENORPHINE [J].
LEWIS, JW .
DRUG AND ALCOHOL DEPENDENCE, 1985, 14 (3-4) :363-372